Dosing & Uses
Dosage Forms & Strengths
packet
- 4g
powder for oral suspension
- 4g/dose (231g)
- 4g/dose (378g)
- 4g/dose (210g)
Hyperlipidemia
4 g PO q12-24hr; increase gradually over ≥1 month intervals
Maintenance: 8-16 g/day PO divided q12hr; not to exceed 24 g/day
Overdose: Symptoms include gastrointestinal (GI) obstruction; treatment is supportive
Dosing Modifications
Renal impairment: Supplemental doses not necessary with peritoneal dialysis (PD) or hemodialysis (HD)
Administration
Always mix with fluids or food
Take before or with meals
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (1)
- mycophenolate
cholestyramine decreases levels of mycophenolate by inhibition of GI absorption. Applies only to oral form of both agents. Contraindicated. Cholestyramine binds bile acids and reduces mycophenolic acid exposure.
Serious - Use Alternative (1)
- warfarin
cholestyramine decreases effects of warfarin by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Cholestyramine and vitamin K antagonists should be administered 3-4 hr apart and monitor patients closely for reduced vitamin K antagonist effects.
Monitor Closely (64)
- amiodarone
cholestyramine decreases levels of amiodarone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- atorvastatin
cholestyramine decreases levels of atorvastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- bendroflumethiazide
cholestyramine decreases levels of bendroflumethiazide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- beta carotene
cholestyramine decreases levels of beta carotene by drug binding in GI tract. Use Caution/Monitor.
- budesonide
cholestyramine decreases levels of budesonide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- calcifediol
cholestyramine will decrease the level or effect of calcifediol by drug binding in GI tract. Modify Therapy/Monitor Closely. Dose adjustment of calcifediol may be required, and serum total 25-hydroxyvitamin D, intact PTH, and serum calcium concentrations should be monitored closely if cholestyramine is initiated or discontinued.
- chlorothiazide
cholestyramine decreases levels of chlorothiazide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- chlorthalidone
cholestyramine decreases levels of chlorthalidone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- cholic acid
cholestyramine will decrease the level or effect of cholic acid by drug binding in GI tract. Use Caution/Monitor. Take cholic acid at least 1 hr before or 4-6 hr (or as great an interval as possible) after a bile acid binding resin.
- cortisone
cholestyramine decreases levels of cortisone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- deferasirox
cholestyramine decreases levels of deferasirox by Other (see comment). Use Caution/Monitor. Comment: Avoid concomitant use of cholestyramine with deferasirox. If co-administration is required then consider increasing initial dose of deferasirox to 30 mg/kg and monitor serum ferritin levels and clinical response.
- deflazacort
cholestyramine decreases levels of deflazacort by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- demeclocycline
cholestyramine decreases levels of demeclocycline by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- dexamethasone
cholestyramine decreases levels of dexamethasone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- diclofenac
cholestyramine decreases levels of diclofenac by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- digoxin
cholestyramine decreases levels of digoxin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- doxercalciferol
cholestyramine decreases levels of doxercalciferol by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. (Vitamin D analog).
- doxycycline
cholestyramine decreases levels of doxycycline by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- ezetimibe
cholestyramine decreases levels of ezetimibe by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2-4 hours.
- fenofibrate
cholestyramine decreases levels of fenofibrate by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- fenofibrate micronized
cholestyramine decreases levels of fenofibrate micronized by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- fenofibric acid
cholestyramine decreases levels of fenofibric acid by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- fludrocortisone
cholestyramine decreases levels of fludrocortisone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- fluvastatin
cholestyramine decreases levels of fluvastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- furosemide
cholestyramine decreases levels of furosemide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- gemfibrozil
cholestyramine decreases levels of gemfibrozil by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- hydrochlorothiazide
cholestyramine decreases levels of hydrochlorothiazide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- hydrocortisone
cholestyramine decreases levels of hydrocortisone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- imipramine
cholestyramine decreases levels of imipramine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- indapamide
cholestyramine decreases levels of indapamide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- leflunomide
cholestyramine decreases levels of leflunomide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- levothyroxine
cholestyramine decreases levels of levothyroxine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Bile acid sequestrants are known to decrease levothyroxine absorption. Separate adminisration by 4 hr or monitor thyrotropin (TSH) levels.
- liothyronine
cholestyramine decreases levels of liothyronine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- lomitapide
cholestyramine decreases levels of lomitapide by drug binding in GI tract. Use Caution/Monitor. Separate lomitapide and administration of bile acid sequestrants by at least 4 hours; bile acid sequestrants can interfere with the absorption of oral medications.
- lovastatin
cholestyramine decreases levels of lovastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- meloxicam
cholestyramine decreases levels of meloxicam by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- methotrexate
cholestyramine decreases levels of methotrexate by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. To minimize drug interactions, administer other drugs at least 1 hour before or at least 4-6 hours after the administration of cholestyramine.
- methyclothiazide
cholestyramine decreases levels of methyclothiazide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- methylprednisolone
cholestyramine decreases levels of methylprednisolone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- metolazone
cholestyramine decreases levels of metolazone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- metronidazole
cholestyramine decreases levels of metronidazole by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- minocycline
cholestyramine decreases levels of minocycline by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- niacin
cholestyramine decreases levels of niacin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- obeticholic acid
cholestyramine will decrease the level or effect of obeticholic acid by drug binding in GI tract. Modify Therapy/Monitor Closely. Administer obeticholic acid at least 4 hr before or 4 hr after taking a bile acid binding resins.
- odevixibat
cholestyramine will decrease the level or effect of odevixibat by drug binding in GI tract. Modify Therapy/Monitor Closely. Administer bile acid sequestrants 4 hr before or after odevixibat.
- omadacycline
cholestyramine will decrease the level or effect of omadacycline by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Monitor for decreased effects of tetracyclines if coadministered with a bile acid sequestrant. Separate doses 2 or more hours if these agents are used concomitantly.
- oxytetracycline
cholestyramine decreases levels of oxytetracycline by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- paricalcitol
cholestyramine decreases levels of paricalcitol by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. (Vitamin D analog).
- piroxicam
cholestyramine decreases levels of piroxicam by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- pitavastatin
cholestyramine decreases levels of pitavastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- pravastatin
cholestyramine decreases levels of pravastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- prednisolone
cholestyramine decreases levels of prednisolone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- prednisone
cholestyramine decreases levels of prednisone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- raloxifene
cholestyramine decreases levels of raloxifene by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- rosuvastatin
cholestyramine decreases levels of rosuvastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- sarecycline
cholestyramine will decrease the level or effect of sarecycline by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Monitor for decreased effects of tetracyclines if coadministered with a bile acid sequestrant. Separate doses by 2 or more hours if coadministered.
- simvastatin
cholestyramine decreases levels of simvastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- spironolactone
cholestyramine, spironolactone. unspecified interaction mechanism. Use Caution/Monitor. Hyperkalemic metabolic acidosis reported when coadministered.
- tetracycline
cholestyramine decreases levels of tetracycline by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- thyroid desiccated
cholestyramine decreases levels of thyroid desiccated by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- tinidazole
cholestyramine will decrease the level or effect of tinidazole by Other (see comment). Use Caution/Monitor. Coadministration of cholestyramine with tinidazole may decrease absorption of tinidazole. Advise to separate dosing regimens for cholestyramine and tinidazole to minimize any potential effect on the oral bioavailability of tinidazole.
- triamcinolone acetonide injectable suspension
cholestyramine decreases levels of triamcinolone acetonide injectable suspension by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- valproic acid
cholestyramine decreases levels of valproic acid by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- vitamin D
cholestyramine will decrease the level or effect of vitamin D by Other (see comment). Use Caution/Monitor. Bile acid sequestrants may decrease the absorption of fat-soluble vitamins. Administer vitamin supplementation at least 4 hours prior to cholestyramine.
Minor (7)
- acetaminophen
cholestyramine decreases levels of acetaminophen by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- acetaminophen IV
cholestyramine decreases levels of acetaminophen IV by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- acetaminophen rectal
cholestyramine decreases levels of acetaminophen rectal by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- chenodiol
cholestyramine decreases levels of chenodiol by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- ursodiol
cholestyramine decreases effects of ursodiol by pharmacodynamic antagonism. Minor/Significance Unknown.
- vitamin A
cholestyramine decreases levels of vitamin A by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown. (Vitamin A).
- vitamin K1 (phytonadione)
cholestyramine decreases levels of vitamin K1 (phytonadione) by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown. (Vitamin K).
Adverse Effects
Frequency Not Defined
Belching
Constipation
Dental erosion
Diarrhea
Duodenal ulcer bleeding
Flatulence
Gallstones
Heartburn
Hypoprothrombinemia
Malabsorption of fat-soluble vitamins
Nausea and vomiting
Pancreatitis
Perianal irritation
Rectal pain
Steatorrhea
Stomach pain
Weight gain or loss
Warnings
Contraindications
Hypersensitivity to bile-sequestering resins
Complete biliary obstruction
Cautions
Use with caution in renal impairment
Volume depletion
Concomitant spironolactone therapy
Not for use with baseline fasting triglyceride levels ≥300 mg/dL or type III hyperlipoproteinemia; use with caution in patients with triglyceride levels 250-299 mg/dL; perform fasting lipid panel in 4-6weeks after initiation; discontinue use if triglycerides are >400 mg/dL; secondary causes of hyperlipidemia must be ruled out before therapy is initiated
Not to be used as monotherapy in hypertriglyceridemia
With prolonged use, increased risk of bleeding because of hypoprothrombinemia from vitamin K deficiency
May interfere with fat absorption and decrease absorption of fat-soluble vitamins (A, D, E, K)
May exacerbate preexisting constipation (initiate therapy at lower dosage in patients with history of constipation)
Special care must be taken to avoid constipation in patients with symptomatic coronary heart disease
Always mix with water or fluids; never ingest dry powder
Some formulations contain phenylalanine
Because of large quantities of chloride ion released from resin (which may lead to hyperchloremic acidosis and increase urinary calcium excretion on prolonged use), it may be advisable to reduce chloride intake
Take other drugs at least 1 hour before or 4-6 hours after taking cholestyramine to minimize possible interference with absorption
Pregnancy & Lactation
Pregnancy category: C
Lactation: Drug does not enter breast milk; use with caution because of potential vitamin loss in mother
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Forms complex with bile acids that is not absorbed through intestine; inhibits enterohepatic reuptake of intestinal bile salts, and this, in turn, increases fecal loss of bile salt-bound LDL and consequently reduces serum cholesterol in patients with primary hypercholesterolemia
Absorption
Not absorbed
Peak effect: 21 days
Metabolism
Not metabolized
Elimination
Excretion: Feces (insoluble complex with bile acids)
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